EP0934287A4 - Heterocyclic esters and amides - Google Patents

Heterocyclic esters and amides

Info

Publication number
EP0934287A4
EP0934287A4 EP97938449A EP97938449A EP0934287A4 EP 0934287 A4 EP0934287 A4 EP 0934287A4 EP 97938449 A EP97938449 A EP 97938449A EP 97938449 A EP97938449 A EP 97938449A EP 0934287 A4 EP0934287 A4 EP 0934287A4
Authority
EP
European Patent Office
Prior art keywords
amides
heterocyclic esters
heterocyclic
esters
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP97938449A
Other languages
German (de)
French (fr)
Other versions
EP0934287A1 (en
EP0934287B1 (en
Inventor
Jia-He Li
Gregory S Hamilton
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Gliamed Inc
Original Assignee
Guilford Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Guilford Pharmaceuticals Inc filed Critical Guilford Pharmaceuticals Inc
Publication of EP0934287A1 publication Critical patent/EP0934287A1/en
Publication of EP0934287A4 publication Critical patent/EP0934287A4/en
Application granted granted Critical
Publication of EP0934287B1 publication Critical patent/EP0934287B1/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D267/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02Seven-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/04Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D277/06Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D279/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/101,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/121,4-Thiazines; Hydrogenated 1,4-thiazines not condensed with other rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
EP97938449A 1996-09-25 1997-08-20 Heterocyclic esters and amides Expired - Lifetime EP0934287B1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/719,947 US5801187A (en) 1996-09-25 1996-09-25 Heterocyclic esters and amides
US719947 1996-09-25
PCT/US1997/014624 WO1998013355A1 (en) 1996-09-25 1997-08-20 Heterocyclic esters and amides

Publications (3)

Publication Number Publication Date
EP0934287A1 EP0934287A1 (en) 1999-08-11
EP0934287A4 true EP0934287A4 (en) 2000-01-12
EP0934287B1 EP0934287B1 (en) 2009-05-27

Family

ID=24892040

Family Applications (1)

Application Number Title Priority Date Filing Date
EP97938449A Expired - Lifetime EP0934287B1 (en) 1996-09-25 1997-08-20 Heterocyclic esters and amides

Country Status (24)

Country Link
US (4) US5801187A (en)
EP (1) EP0934287B1 (en)
JP (1) JP2001502668A (en)
KR (1) KR20000048589A (en)
CN (1) CN1234795A (en)
AR (1) AR009749A1 (en)
AT (1) ATE432266T1 (en)
AU (1) AU732194C (en)
BG (1) BG103232A (en)
BR (1) BR9712834A (en)
CA (1) CA2263925A1 (en)
CZ (1) CZ66099A3 (en)
DE (1) DE69739422D1 (en)
EA (1) EA199900140A1 (en)
HU (1) HUP0000969A3 (en)
ID (1) ID19588A (en)
IL (1) IL128675A (en)
NO (1) NO991433L (en)
NZ (1) NZ334186A (en)
PA (1) PA8438501A1 (en)
PL (1) PL332183A1 (en)
SK (1) SK26699A3 (en)
WO (1) WO1998013355A1 (en)
ZA (1) ZA977901B (en)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6291510B1 (en) 1995-06-07 2001-09-18 Gpi Nil Holdings, Inc. Small molecule inhibitors of rotamase enzyme activity
US6509477B1 (en) 1998-11-12 2003-01-21 Guilford Pharmaceuticals Inc. Small molecule inhibitors of rotamase enzyme activity
US5859031A (en) * 1995-06-07 1999-01-12 Gpi Nil Holdings, Inc. Small molecule inhibitors of rotamase enzyme activity
US5801187A (en) 1996-09-25 1998-09-01 Gpi-Nil Holdings, Inc. Heterocyclic esters and amides
US6218424B1 (en) * 1996-09-25 2001-04-17 Gpi Nil Holdings, Inc. Heterocyclic ketone and thioester compounds and uses
US5935989A (en) 1996-12-31 1999-08-10 Gpi Nil Holdings Inc. N-linked ureas and carbamates of heterocyclic thioesters
JP2002515050A (en) 1996-12-31 2002-05-21 ジーピーアイ エヌアイエル ホールディングス インコーポレイテッド N-linked ureas and carbamates of heterocyclic thioesters
US5721256A (en) * 1997-02-12 1998-02-24 Gpi Nil Holdings, Inc. Method of using neurotrophic sulfonamide compounds
US5846979A (en) 1997-02-28 1998-12-08 Gpi Nil Holdings, Inc. N-oxides of heterocyclic esters, amides, thioesters, and ketones
CA2333997A1 (en) 1998-06-02 1999-12-09 Bristol-Myers Squibb Company Neurotrophic difluoroamide agents
EP1085853A1 (en) * 1998-06-03 2001-03-28 GPI NIL Holdings, Inc. Heterocyclic ester and amide hair growth compositions and uses
US6331537B1 (en) 1998-06-03 2001-12-18 Gpi Nil Holdings, Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
AU1708099A (en) 1998-06-03 1999-12-20 Amgen, Inc. N-linked sulfonamides of n-heterocyclic carboxylic acids or carboxylic acid isosteres
HUP0200637A3 (en) 1998-07-17 2003-05-28 Agouron Pharmaceuticals Inc La Compounds, compositions, and their use for stimulating neuronal growth and elongation
US6686357B1 (en) 1999-07-15 2004-02-03 Pfizer, Inc. FKBP inhibitors
GB9815696D0 (en) * 1998-07-20 1998-09-16 Pfizer Ltd Heterocyclics
GB9815880D0 (en) * 1998-07-21 1998-09-16 Pfizer Ltd Heterocycles
US6376517B1 (en) * 1998-08-14 2002-04-23 Gpi Nil Holdings, Inc. Pipecolic acid derivatives for vision and memory disorders
WO2000009108A2 (en) * 1998-08-14 2000-02-24 Gpi Nil Holdings, Inc. Compositions and uses for vision and memory disorders
US7338976B1 (en) * 1998-08-14 2008-03-04 Gpi Nil Holdings, Inc. Heterocyclic esters or amides for vision and memory disorders
US6337340B1 (en) * 1998-08-14 2002-01-08 Gpi Nil Holdings, Inc. Carboxylic acids and isosteres of heterocyclic ring compounds having multiple heteroatoms for vision and memory disorders
US6399648B1 (en) * 1998-08-14 2002-06-04 Gpi Nil Holdings, Inc. N-oxides of heterocyclic ester, amide, thioester, or ketone for vision and memory disorders
US6462072B1 (en) 1998-09-21 2002-10-08 Gpi Nil Holdings, Inc. Cyclic ester or amide derivatives
US6307049B1 (en) 1998-09-30 2001-10-23 The Procter & Gamble Co. Heterocyclic 2-substituted ketoamides
US6300341B1 (en) 1998-09-30 2001-10-09 The Procter & Gamble Co. 2-substituted heterocyclic sulfonamides
US6228872B1 (en) 1998-11-12 2001-05-08 Bristol-Myers Squibb Company Neurotrophic diamide and carbamate agents
MXPA02000330A (en) * 1999-07-09 2004-05-21 Johnson & Johnson Neurotrophic pyrrolidines and piperidines, and related compositions and methods.
WO2001004091A1 (en) 1999-07-09 2001-01-18 Ortho-Mcneil Pharmaceutical, Inc. Neurotrophic 2-azetidinecarboxylic acid derivatives, and related compositions and methods
WO2001004090A2 (en) * 1999-07-09 2001-01-18 Ortho-Mcneil Pharmaceutical, Inc. Neurotrophic tetrahydroisoquinolines and tetrahydrothienopyridines, and related compositions and methods
JP2003508512A (en) 1999-09-08 2003-03-04 ギルフォード ファーマシュウティカルズ インコーポレイテッド Non-peptidic cyclophilin binding compounds and their uses
ATE335524T1 (en) * 1999-11-12 2006-09-15 Alcon Inc USE OF NEUROPHILIN LIGANDS TO TREAT EYE DISEASES
US6417189B1 (en) 1999-11-12 2002-07-09 Gpi Nil Holdings, Inc. AZA compounds, pharmaceutical compositions and methods of use
US7253169B2 (en) 1999-11-12 2007-08-07 Gliamed, Inc. Aza compounds, pharmaceutical compositions and methods of use
DOP2000000107A (en) 1999-12-01 2002-09-16 Agouron Pharmaceutical Inc COMPOUNDS, COMPOSITIONS AND METHODS TO STIMULATE THE GROWTH AND LENGTH OF NEURONS
US6818643B1 (en) 1999-12-08 2004-11-16 Bristol-Myers Squibb Company Neurotrophic bicyclic diamides
CA2393466C (en) 1999-12-21 2010-01-19 Gpi Nil Holdings, Inc. Hydantoin derivative compounds, pharmaceutical compositions, and methods of using same
EP1363620A2 (en) * 2000-12-22 2003-11-26 Pintex Pharmaceuticals, Inc. Use of fredericamycin and its derivatives in the treatment of pin1-associated states
US20030185754A1 (en) * 2001-01-16 2003-10-02 Genset, S.A. Treatment of CNS disorders using D-amino acid oxidase and D-aspartate oxidase antagonists
US20030166554A1 (en) * 2001-01-16 2003-09-04 Genset, S.A. Treatment of CNS disorders using D-amino acid oxidase and D-aspartate oxidase antagonists
WO2002059080A2 (en) 2001-01-25 2002-08-01 Guilford Pharmaceuticals Inc. Trisubstituted carbocyclic cyclophilin binding compounds and their use
US6593362B2 (en) 2001-05-21 2003-07-15 Guilford Pharmaceuticals Inc. Non-peptidic cyclophilin binding compounds and their use
CA2449019A1 (en) * 2001-05-29 2002-12-05 Guilford Pharmaceuticals Inc. Method for treating nerve injury caused by surgery
CN1240691C (en) 2001-12-06 2006-02-08 中国人民解放军军事医学科学院毒物药物研究所 Substituted penta azacylo compounds and their use for preventing and treating nervous retrogression disease
US20060089400A1 (en) * 2002-05-03 2006-04-27 The Vernalis Group Of Companies Novel spiro ketone and carboxylic acid derivatives as specific inhibitors for (po3h2) ser/(po3h2)thr-pro-specific peptidyl-prolylcis/trans-isomerases
US20060189551A1 (en) * 2004-10-04 2006-08-24 Duke University Combination therapies for fungal pathogens
US20050148669A1 (en) * 2004-10-21 2005-07-07 Daniel Amato Amino acid esters as nutrient supplements and methods of use
GB0724625D0 (en) * 2007-12-18 2008-01-30 Glaxo Group Ltd Novel compounds

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1559851A (en) * 1968-01-30 1969-03-14

Family Cites Families (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3385918A (en) * 1962-12-01 1968-05-28 Bx Plastics Ltd Extrusion process and apparatus for isotactic polypropylene
IL58849A (en) * 1978-12-11 1983-03-31 Merck & Co Inc Carboxyalkyl dipeptides and derivatives thereof,their preparation and pharmaceutical compositions containing them
EP0038117A1 (en) 1980-03-10 1981-10-21 University Of Miami Methods for preparing anti-hypertensive agents
US4310461A (en) * 1980-06-23 1982-01-12 E. R. Squibb & Sons, Inc. Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids
US4578474A (en) * 1980-06-23 1986-03-25 E. R. Squibb & Sons, Inc. Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids
US4390695A (en) 1980-06-23 1983-06-28 E. R. Squibb & Sons, Inc. Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids
US4950649A (en) * 1980-09-12 1990-08-21 University Of Illinois Didemnins and nordidemnins
EP0048159A3 (en) * 1980-09-17 1982-05-12 University Of Miami Novel carboxyalkyl peptides and thioethers and ethers of peptides as antihypertensive agents
LU88621I2 (en) * 1980-10-23 1995-09-01 Schering Corp Sandopril
ZA817261B (en) * 1980-10-23 1982-09-29 Schering Corp Carboxyalkyl dipeptides,processes for their production and pharmaceutical compositions containing them
ZA826022B (en) 1981-08-21 1983-08-31 Univ Miami Novel complex amido and imido derivatives of carboxyalkyl peptides and thioethers and ethers of peptides
EP0088350B1 (en) 1982-03-08 1985-02-20 Schering Corporation Carboxyalkyl dipeptides, processes for their production and pharmaceutical compositions containing them
US4531964A (en) * 1982-09-13 1985-07-30 Nippon Kayaku Kabushiki Kaisha Heterocyclic compound and a herbicidal composition containing said compound
US4574079A (en) 1983-05-27 1986-03-04 Gavras Haralambos P Radiolabeled angiotensin converting enzyme inhibitors for radiolabeling mammalian organ sites
US4593102A (en) 1984-04-10 1986-06-03 A. H. Robins Company, Inc. N-[(amino)alkyl]-1-pyrrolidine, 1-piperidine and 1-homopiperidinecarboxamides (and thiocarboxamides) with sulfur linked substitution in the 2, 3 or 4-position
DE3508251A1 (en) 1985-03-08 1986-09-11 Merck Patent Gmbh, 6100 Darmstadt Dipeptides
CN86101850A (en) * 1985-03-22 1987-02-04 森得克斯(美国)有限公司 N, the manufacture method and the purposes of N '-dialkyl group guanidine radicals dipeptides
ATE70048T1 (en) 1986-09-10 1991-12-15 Syntex Inc SELECTIVE AMIDINATION OF DIAMINES.
DE3643012A1 (en) * 1986-12-17 1988-06-30 Hoechst Ag 2,3-DISUBSTITUTED ISOXAZOLIDINE, METHOD FOR THE PRODUCTION THEREOF, THE CONTAINERS THEREOF AND THEIR USE
IT1206078B (en) 1987-06-03 1989-04-14 Polifarma Spa PROCEDURE FOR THE PRODUCTION OF 3-INDOLPIRUVIC ACID AND ITS DERIVATIVES THEIR PHARMACEUTICAL USE
US5187156A (en) * 1988-03-16 1993-02-16 Fujisawa Pharmaceutical Co., Ltd. Peptide compounds, processes for preparation thereof and pharmaceutical composition comprising the same
IL90872A0 (en) * 1988-07-08 1990-02-09 Smithkline Beckman Corp Retroviral protease binding peptides
DE3931051A1 (en) * 1988-09-22 1990-03-29 Hoechst Ag New herbicidal amine salts of herbicidal acids
EP0378318A1 (en) 1989-01-11 1990-07-18 Merck & Co. Inc. Process for synthesis of FK-506 and tricarbonyl intermediates
US5359138A (en) * 1989-04-15 1994-10-25 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Poststatin and related compounds or salts thereof
US5162500A (en) * 1989-04-15 1992-11-10 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Poststatin and related compounds or salts thereof
US5164525A (en) 1989-06-30 1992-11-17 Merck & Co., Inc. Synthetic process for fk-506 type macrolide intermediates
NZ234883A (en) * 1989-08-22 1995-01-27 Merck Frosst Canada Inc Quinolin-2-ylmethoxy indole derivatives, preparation and pharmaceutical compositions thereof
GB8922026D0 (en) * 1989-09-29 1989-11-15 Pharma Mar Sa Novel anti-viral and cytotoxic agent
US5115098A (en) * 1990-02-28 1992-05-19 President And Fellows Of Harvard College End-blocked peptides inhibiting binding capacity of gp120
JPH04211648A (en) 1990-07-27 1992-08-03 Nippon Kayaku Co Ltd Keto-acid amide derivative
DE4015255A1 (en) * 1990-05-12 1991-11-14 Hoechst Ag OXALYL-AMINOSA-E-LEED DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS A MEDICAMENT FOR INHIBITING THE PROLYL HYDROXYLASE
US5192773A (en) * 1990-07-02 1993-03-09 Vertex Pharmaceuticals, Inc. Immunosuppressive compounds
WO1992003472A1 (en) * 1990-08-24 1992-03-05 The Upjohn Company Peptides containing amino-polyols as transition-state mimics
AU8727491A (en) * 1990-08-29 1992-03-30 Vertex Pharmaceuticals Incorporated Modified di- and tripeptidyl immunosuppressive compounds
GB2247456A (en) 1990-09-03 1992-03-04 Fujisawa Pharmaceutical Co Tetrahydropyrane compounds, a process for their production and a pharmaceutical composition containing the same
JPH04149166A (en) 1990-10-12 1992-05-22 Nippon Kayaku Co Ltd Novel keto acid amide derivative
AU1677092A (en) * 1991-03-20 1992-10-21 Vertex Pharmaceuticals Incorporated Tetrahydroxyalkane derivatives as inhibitors of hiv aspartyl protease
IT1245712B (en) 1991-04-09 1994-10-14 Boehringer Mannheim Italia USEFUL HETEROCYCLIC AMINES THERAPY OF ASTHMA AND AIRWAY INFLAMMATION
US5147877A (en) * 1991-04-18 1992-09-15 Merck & Co. Inc. Semi-synthetic immunosuppressive macrolides
WO1992019745A1 (en) * 1991-05-08 1992-11-12 Vertex Pharmaceuticals Incorporated Rfkbp: a novel prolyl isomerase and rapamycin/fk506 binding protein
EP0584223B1 (en) * 1991-05-09 1999-08-11 Vertex Pharmaceuticals Incorporated Novel immunosuppressive compounds
MX9202466A (en) * 1991-05-24 1994-06-30 Vertex Pharma NOVELTY IMMUNOSUPPRESSIVE COMPOUNDS.
DE4120695A1 (en) 1991-06-22 1992-12-24 Bayer Ag OPTICALLY ACTIVE SULFURIZED AMINO ACID DERIVATIVES, THEIR PRODUCTION, THEIR POLYMERIZATION TO OPTICALLY ACTIVE POLYMERS AND THEIR USE
JPH05178824A (en) 1991-08-05 1993-07-20 Takeda Chem Ind Ltd Asparagine derivative and its use
WO1993007269A1 (en) * 1991-10-11 1993-04-15 Vertex Pharmaceuticals Incorporated ISOLATION OF AN Mr 52,000 FK506 BINDING PROTEIN AND MOLECULAR CLONING OF A CORRESPONDING HUMAN cDNA
IL103394A0 (en) 1991-10-11 1993-03-15 Ciba Geigy Pyrimidinyl and triazinyl ethers and thioethers,their preparation and their use as herbicides
WO1993013066A1 (en) * 1991-12-20 1993-07-08 Syntex (U.S.A.) Inc. Cyclic amides of 3-amino-2-hydroxy-carboxylic acids as hiv-protease inhibitors
CA2091194A1 (en) * 1992-04-08 1993-10-09 Richard D. Connell 2-oxo-ethyl derivatives as immunosuppressants
AU4388893A (en) * 1992-05-20 1993-12-13 Vertex Pharmaceuticals Incorporated Method of detecting tissue-specific FK506 binding protein messenger RNAs and uses thereof
IT1254373B (en) 1992-05-29 1995-09-14 HETEROPROSTANOIDS, PROCEDURE FOR THEIR PREPARATION AND THEIR EMPLOYE THERAPEUTIC.
US5334719A (en) * 1992-06-17 1994-08-02 Merck Frosst Canada, Inc. Bicyclic(azaaromatic)indoles as inhibitors of leukotriene bisynthesis
IS2334B (en) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl protease inhibitor of a new class of sulfonamides
NZ314207A (en) * 1992-09-28 2000-12-22 Vertex Pharma 1-(2-Oxoacetyl)-piperidine-2-carboxylic acid derivatives as multi drug resistant cancer cell sensitizers
WO1994013629A1 (en) * 1992-12-11 1994-06-23 Vertex Pharmaceuticals Incorporated Mannitol derivatives and their use as inhibitors of aspartyl protease
DE4302860A1 (en) * 1993-01-22 1994-08-04 Chemie Linz Deutschland N-Cyclic and N, N'dicyclic ureas
US5385918A (en) * 1993-02-09 1995-01-31 Miles Inc. Aminomethylene-peptides as immunosuppressants
US5252579A (en) * 1993-02-16 1993-10-12 American Home Products Corporation Macrocyclic immunomodulators
US5319098A (en) * 1993-05-18 1994-06-07 Celgene Corporation Process for the stereoselective preparation of L-alanyl-L-proline
US5798355A (en) 1995-06-07 1998-08-25 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity
IT1270882B (en) 1993-10-05 1997-05-13 Isagro Srl FUNGICIDE-BASED OLIGOPEPTIDES
EP0677039B1 (en) * 1993-11-04 1999-03-10 Abbott Laboratories Cyclobutane derivatives as inhibitors of squalene synthetase and protein farnesyltransferase
CA2183653A1 (en) * 1994-03-07 1995-09-14 Roger Dennis Tung Sulphonamide derivatives as aspartyl protease inhibitors
US5744485A (en) * 1994-03-25 1998-04-28 Vertex Pharmaceuticals Incorporated Carbamates and ureas as modifiers of multi-drug resistance
US6057119A (en) * 1994-06-17 2000-05-02 Vertex Pharmaceuticals, Incorporated Crystal structure and mutants of interleukin-1β converting enzyme
US5716929A (en) * 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
ATE299145T1 (en) * 1994-08-18 2005-07-15 Ariad Gene Therapeutics Inc NEW MULTIMERIZING REAGENT
US5543423A (en) * 1994-11-16 1996-08-06 Vertex Pharmaceuticals, Incorporated Amino acid derivatives with improved multi-drug resistance activity
IL115685A (en) * 1994-11-16 2000-08-31 Vertex Pharma Amino acid derivatives pharmaceutical compositions containing the same and processes for the preparation thereof
US5621108A (en) 1994-12-05 1997-04-15 Trustees Of The University Of Pennsylvania Processes and intermediates for preparing macrocycles
US5859031A (en) 1995-06-07 1999-01-12 Gpi Nil Holdings, Inc. Small molecule inhibitors of rotamase enzyme activity
US5696135A (en) 1995-06-07 1997-12-09 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity effective at stimulating neuronal growth
US5614547A (en) 1995-06-07 1997-03-25 Guilford Pharmaceuticals Inc. Small molecule inhibitors of rotamase enzyme
US6037370A (en) * 1995-06-08 2000-03-14 Vertex Pharmaceuticals Incorporated Methods and compositions for stimulating neurite growth
US5801197A (en) 1995-10-31 1998-09-01 Gpi Nil Holdings, Inc. Rotamase enzyme activity inhibitors
US5717092A (en) 1996-03-29 1998-02-10 Vertex Pharmaceuticals Inc. Compounds with improved multi-drug resistance activity
US5801187A (en) 1996-09-25 1998-09-01 Gpi-Nil Holdings, Inc. Heterocyclic esters and amides
US5786378A (en) 1996-09-25 1998-07-28 Gpi Nil Holdings, Inc. Heterocyclic thioesters
US5721256A (en) 1997-02-12 1998-02-24 Gpi Nil Holdings, Inc. Method of using neurotrophic sulfonamide compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1559851A (en) * 1968-01-30 1969-03-14

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
B. AKERMARK, N.-G. JOHANSSON: "Synthesis of strained heterocyclic rings. I. 2-Hydroxy-beta-lactams and 4-oxazolidinones by photocyclization of 2-oxoamides", TETRAHEDRON LETTERS, no. 5, 1969, pages 371 - 372, XP002124578 *
D. M. BRUNWIN, G. LOWE: "Total Synthesis of Nuclear Analogues of 7-Methylcephalosporin", J. CHEM. SOC. PERKIN TRNS. I, 1973, pages 1321 - 1328, XP002124580 *
K. R. HENERY-LOGAN, C. G. CHEN: "Synthesis of oxygen analogs of the penicillins. I. Photocyclization of 2-oxoamides to 3-carbomethoxy-6-hydroxypenams", TETRAHEDRON LETTERS, no. 13, 1973, pages 1103 - 1104, XP002124579 *
L. V. DUNKERTON, R. M. AHMED: "Synthetic approaches to bicyclomycin I. Preparation of monocyclic intermediates by retrograde Michael cleavage of 6-alkyl-6-methoxyhexahydro-3H-thiazolo[3,4-a]pyrazine-5,8-diones", TETRAHEDRON LETTERS, vol. 21, 1980, pages 1803 - 1806, XP002124581 *
Y. INAMORI ET AL.: "Synthesis of Methyl and ethyl 3-Alkylthiazolidine-4(R)-carboxylates and Their Roots Inhibition of the Growth of Brassica campestris", BIOSCI. BIOTECHNOL. BIOCHEM., vol. 58, no. 6, 1994, pages 1150 - 1152, XP002124582 *

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